烟曲霉素(fumagillin )
烟曲霉素(fumagillin )由烟曲霉(Aspergillus fumigatus)的发酵培养液中分离得到的一种抗生素。
黄色针状结晶。熔点194~195℃。旋光度[α]D25-26.6°(c=1,乙醇)。几乎不溶于水、稀酸类、饱和烃,溶于乙醇等有机溶剂。既具抗生素活性,又有致癌作用。
Fumagillin is a complex biomolecule and used as an antimicrobial agent. It was isolated in 1949 from the microbial organism Aspergillus fumigatus.
In animals
It was originally used against microsporidial parasites Nosema apis and Nosema ceranae infections in honey bees.
Some studies found it to be effective against some myxozoan parasites, including Myxobolus cerebralis, an important parasite of fish; however, in the more rigorous tests required for U.S. Food and Drug Administration approval, it was ineffective.
There are reports that fumagillin controls Nosema ceranae, which has recently been hypothesized as a possible cause of colony collapse disorder.
Fumagillin is also investigated as an inhibitor of malaria parasite growth.
In humans
Fumagillin has been used in the treatment of microsporidiosis. It is also an amebicide.
Fumagillin can block blood vessel formation by binding to an enzyme called methionine aminopeptidase 2. and for this reason, the compound, together with semisynthetic derivatives, are investigated as a angiogenesis inhibitor in the treatment of cancer.
Preliminary clinical trials are being conducted by Zafgen into using the fumagillin analog beloranib for weight loss.
Fumagillin and the related fumagillol (the hydrolysis product) have been a target in total synthesis, with several reported successful strategies, racemic, asymmetric and formal.